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Gabexate mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gabexate mesylate图片
CAS NO:56974-61-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
50mg电议

产品介绍
Gabexate mesylate 是一种因子 X 抑制剂;丝氨酸蛋白酶抑制剂。
Cas No.56974-61-9
别名甲磺酸加贝酯; FOY
化学名ethyl 4-[6-(diaminomethylideneamino)hexanoyloxy]benzoate;methanesulfonic acid
Canonical SMILESCCOC(=O)C1=CC=C(C=C1)OC(=O)CCCCCN=C(N)N.CS(=O)(=O)O
分子式C16H23N3O4.CH4O3S
分子量417.48
溶解度≥ 18.2 mg/mL in DMSO, ≥ 99.8 mg/mL in EtOH, ≥ 102.4 mg/mL in Water
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Gabexate mesylate is a non-antigenic synthetic inhibitor of trypsin-like serine proteinases with Ki values of 3.4nM and 180nM, respectively for human tryptase and bovine tryptase [1].

Gabexate mesylate is a drug used in the treatment of pancreatitis, disseminated intravascular coagulation and as a regional anticoagulant for hemodialysis. Gabexate mesylate is reported to bind to the primary specificity site S1 of human and bovine tryptases. The carbonyl group of gabexate mesylate interacts with the oxyanion binding hole of the enzyme. The tighter binding of gabexate mesylate to human tryptase results in a higher affinity than to bovine tryptase [1].

Gabexate mesylate is also found to inhibit cNOS and iNOS, with Ki values of 150μM and 5mM. It up-regulates iNOS gene expression. In addition, gabexate mesylate inhibits the LPS/IFNγ-induced NO production with EC50 value of 250μM [2].

References:
[1] Erba F, Fiorucci L, Pascarella S, Menegatti E, Ascenzi P, Ascoli F. Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol. 2001 Feb 1;61(3):271-6.
[2] Colasanti M, Persichini T, Venturini G, Menegatti E, Lauro GM, Ascenzi P. Effect of gabexate mesylate (FOY), a drug for serine proteinase-mediated diseases, on the nitric oxide pathway. Biochem Biophys Res Commun. 1998 May 19;246(2):453-6.